The Search for Novel Human Pancreatic α‐Amylase Inhibitors: High‐Throughput Screening of Terrestrial and Marine Natural Product Extracts

Abstract

Specific inhibitors of human pancreatic alpha-amylase (HPA) have potential as oral agents for the control of blood glucose levels in the treatment of diabetes and obesity. In a search for novel inhibitors, a library of 30 000 crude biological extracts of terrestrial and marine origin has been screened. A number of inhibitory extracts were identified, of which the most potent was subjected to bioassay-guided purification. A family of three glycosylated acyl flavonols, montbretins A-C, was thereby identified and characterized as competitive amylase inhibitors, with K(i) values ranging from 8.1-6100 nM. Competitive inhibition by myricetin, which corresponds to the flavone core, and noncompetitive inhibition by a second fragment, ethyl caffeiate, suggest a binding mode for these inhibitors.

Involvement of Calcium ion in Enhancement of antioxidant and antidiabetic Potential of Fenugreek Sprouts

“…Hence the inhibition of these enzymes would minimize the breakdown of starch which may lead to reduction in the postprandial hyperglycemia level. 28 On assessment of invitro antidiabetic activity similar trend was observed in the α-amylase and α-glucosidase inhibitory activity of the fenugreek sprouts primed with different elicitors of Ca 2+ signalling. The α-amylase as well as α-glucosidase inhibitory activity was found to be highest in the sprouts per-treated with calcium chloride and those treated with LaCl 3 and EGTA exhibited decline in the anti-diabetic activity when compared with the control set ( Table 7).…”

Hepatoprotective and antidiabetic activities of Fraxinus angustifolia Vahl extracts in animal models: characterization by high performance liquid chromatography analysis

“…Pancreatic α-amylase catalyzes the initial step in the hydrolysis of starch, a principal source of glucose in the diet (36). Therefore, the inhibition of this enzyme by FAL and FAB extracts would prevent more glucose release in the blood.…”

In vitroandin silicointeraction of porcine α-amylase withVicia fabacrude seed extract and evaluation of antidiabetic activity

“…6 Inhibitors of pancreatic a-amylase delay carbohydrate digestion causing a reduction in the rate of glucose absorption and decrease the postprandial serum glucose levels. 7 Some synthetic drugs are available in the market such as acarbose and miglitol which inhibit a-glucosidase and a-amylase. They are not site-specific, and produce more side effects.…”